This invention relates to a new soft gelatine formulation and process methodology that increases single Coenzyme Q10 molecules presented to the absorption channel of the small intestines.
Coenzyme Q10 (CoQ10) is a large molecular weight lipid compound that is produced in the liver and other organs. The total human body content is 1.4 to 1.8 grams depending on the individual""s age and fitness level. CoQ10 is found in all tissues of the body. It is mostly concentrated in the mitochondria and other organelles that help the body metabolize nutrients into energy. These include organs with high levels of metabolic activity. Organs, whose primary purpose is energy production, tend to store and use CoQ10 in large amounts. Such organs include the heart, liver, and skeletal muscle tissue. The heart and skeletal muscle of an aaverage human contain about 1000 mg of CoQ10. This is in contrast to metabolically inactive body components such as the blood, which only contains about 4 mg of CoQ10. However, blood plays an important role in as a CoQ10 reservoir. Blood helps to transport CoQ10 from endogenous CoQ10 made in the liver and exogenous CoQ10 absorbed from digested food in the intestinal tract. Endogenous CoQ10 accounts for approximately 56 percent of the body""s supply. The remaining 44 percent must be provided through diet and supplementation. These numbers are currently being studied but the latest studies indicate lower endogenous production of CoQ10, which indicates a significant deficiency, in correlation with increased age. Furthermore, certain disease states such as cardio myopathy and high cholesterol levels, which are treated with Statin drugs, seem to deplete endogenous CoQ10 production thereby indicating a need for supplementation. These deficiencies in the nutrient have no relation to daily caloric intake but are indicative of poor vitamin absorption from ingested foods. The body requires the addition of vitamins to aid in the endogenous production of CoQ10; in particular, the B Vitamins play a crucial role in this synthesis.
The human body""s need for CoQ10 varies between individuals. Factors that affect this are age, physical activity, and health. The body uses an estimated 5 to 9 mg per day of CoQ10. This nutrient is essential for life because it is important in the synthesis of energy. The vast majority of energy synthesis occurs in the mitochondria of cells. Here CoQ10 primarily functions as an electron carrier in the Electron Transport Chain where Adenosine Triphosphate (ATP) is synthesized. CoQ10 donates an electron during ATP synthesis and is subsequently oxidized. CoQ10 also can function as an antioxidant during synthesis where oxidation removes its electron making it non-functional for use in ATP synthesis.
Conditions of high metabolic stress deplete the body""s endogenous supply of CoQ10. Because of this, CoQ10 supplementation becomes necessary to meet the body""s requirement for energy production. Under these conditions, dietary supplementation is shown effective provided that the nutrient is delivered in an ideal form. In all of these, an improved soft gelatin formula has been clinically proven, at doses of 30-100 mg/day, to be superior to 60 mg/day dry capsules and previoously available 100 mg/day soft gel formulas.
Research has had difficulty ascertaining the appropriate CoQ10 dose for a diseased individual in comparison to a normal individual. However, the normally recommended dose of 10 to 30 mg/day has been found to be ineffective for individuals with significant deficiencies. For the past 15 years, it has become accepted that poor intestinal absorption of certain forms of CoQ10 limits the effectiveness of its use. Because of this, dosages of 50 mg, 100 mg and even 150 mg are commercially available to the consumer, but at a considerable expense. This deters many persons from supplementing their diets with sufficient CoQ10, a fact that can have deleterious health effects.
Folkers et al. (U.S. Pat. No. 4,824,669) addresses a soft gel capsule with CoQ10 and at least one vegetable oil carrier. This formula was found to increase blood basal levels of CoQ10 to 2.5 g/ml in comparison to 1.6 g/ml from an equivalent 100 mg dose of a dry powder formulation. While many different CoQ10 formulas claim increased intestinal absorption of the nutrient, the data supporting these claims are often inconclusive.
It is clear that a far more efficient formula will produce better results with less CoQ10 than traditional soft gel or dry formulations.
The present invention is made from a stable, non-toxic soft gelatin Coenzyme formulation. The process methodology of Coenzyme Q10, which increases CoenzymeQ10, levels in the intestinal tract and subsequently, in the energy producing organs of the body through carriage in the blood stream. The preferred soft gel formula includes: Coenzyme Q10; medium chain triglycerides or GelOil SC; Vitamin E as mixed tocopherols, which also act as an added antioxidant; Rice Bran Oil; Yellow Beeswax; and Natural Beta carotene. The medium chain triglycerides or GelOil SC work as carriers and serve to increase the bioavailability of the CoQ10 in the gut for a superior absorption formula. The formula need only be administered only twice per day as such is found to be effective and serves the added benefit of reducing the cost to the consumer and ease of use.
The medium chain triglycerides can be replaced with GelOil SC, which is a wetting and suspension agent, those functions in a like manner as the more expensive medium chain triglycerides. Gel Oil SC is a carrier composition which can be obtained from Gattefosse Corporation located at 372 Kinderkamack Road, Westwood, N.J. 07675, U.S.A, and is described as a thixatropic gelatine carrier composition in U.S. Pat. No. 6,365,181 to Matthews. GelOil SC is soybean oil (CAS# 8001-22-7), mixed composition of mono-, di-, tri-glycerides of a 16 to 18 carbon chain length, and polyglycerol oleate (CAS# 9007-48-1). The replacement of the medium chain triglycerides with GelOil SC provides comparable if not better solubility in the intestines and is also a cost effective alternative to the formula, an added benefit to the consumer.
To achieve increased intestinal absorption of CoQ10, the present formulation contains refined soybean oil (Gel Oil SC) or medium chain triglycerides to improve the solubility of the product and provide superior absorption in the intestinal tract. The large molecule oil carriers in the invention allows for superior solubility of the product, which results in greater absorption. Superior absorption of any nutrient is determined by kinetics. The primary carrier used in this invention medium chain triglycerides, or GelOil SC help the large molecule that is CoQ10 improve its absorption kinetics. This is possible because the appropriate carrier can increase the number of single molecules presented to lacteal pores of the intestines into the lymphatic system. The carrier used presents a greater number of molecules that can overcome the three barriers to absorption. The barriers are molecular size, concentration gradient, and membrane thickness. Membrane thickness is sometimes impaired in the elderly through disease states, but this should not affect the availability of CoQ10 in the system. Medium chain triglycerides and GelOil SC are superior to large chain triglycerides. This is because they do not limit the number of single CoQ10 molecules available for absorption through the lacteals. Therefore, using either of these carriers improves the number of single CoQ10 molecules in the intestines. Research has shown that the greater the number of single molecules of CoQ10, the better the chances for improved absorption.
Kishi et al., refers to this when they qualify that the ten isoprenoid units found in CoQ10 make it an extremely water insoluble. However, CoQ10 is a highly lipophilic molecule. They confirm that the bioavailability of the molecule is related directly to its dissolution rate, which the current invention maximizes. The physical chemistry of CoQ10 must be taken into consideration in any formulation, which claims improved absorption. Here, the addition of medium chain triglycerides or GelOil makes this formula extremely bioavailable because it satisfies the molecules lipophilic attraction. This is thought to lead to enhanced absorption potential.
It is therefore an object of the present invention to provide an improved soft gel formulation of CoQ10 and a methodology of processing such that produces a form with significantly greater absorption than prior soft or dry formulations.
Another object is to reduce the cost of providing an effective level of in a human body, whether normal or diseased.
Another object is to provide a soft gel producing process that provides a maximum amount of into the blood stream.
It is the further object of the present invention to provide a soft gel formula and methodology of administration that produces greater absorption in the intestine, which benefits the individual, both in nutrition and cost.
These and other objects and advantages will become apparent to those skilled in the art after considering the following detailed description of the invention.